Category: Cognitive Enhancers

The use of cognition-enhancing drugs by healthy individuals in the absence of a medical indication is one of the most debated topics among neuroscientists, psychiatrists, and physicians who spans a number of issues, including the ethics and fairness of Their use, concerns over adverse effects, and the diversion of prescription drugs for nonmedical uses, among others. Nonetheless, the international sales of cognition-enhancing supplements exceeded US $ 1 trillion in 2015 and the global demand for these compounds is still growing rapidly. And the diversion of prescription drugs for nonmedical uses, among others. [1] [3] [4] Nonetheless, the international sales of cognition-enhancing supplements exceeded US $ 1 trillion in 2015 and the global demand for these compounds is still growing rapidly. And the diversion of prescription drugs for nonmedical uses, among others. Nonetheless, the international sales of cognition-enhancing supplements exceeded US $ 1 trillion in 2015 and the global demand for these compounds is still growing rapidly.

The word nootropic Was coined in 1972 by a Romanian psychologist and chemist, Corneliu E. Giurgea, from the Greek words νους ( us ), or “mind”, and τρέπειν (trepein), meaning to turn or bend.

Availability and prevalence

There are only a few drugs that are known to improve some aspect of cognition. Many more are in different stages of development. [9] The most commonly used class of drug is stimulants , such as caffeine . [10]

These drugs are purportedly used Primarily to treat cognitive or motor function disorders Difficulties Attributable to Such As Alzheimer’s disease , Parkinson’s disease , Huntington’s disease , and ADHD . [ Citation needed ] Some researchers, however, report more widespread use for further research. [11] Nevertheless, intense marketing may not correlate with efficacy . While scientific studies supporting the beneficial effects of Some compounds, manufacturer’s marketing claims for dietary supplements are usually not Formally tested and verified by independent entities. [12]

Use by students

Among students, nootropics-have-been used pour augmenter productivity, DESPITE Their long-term effects lacking conclusive research in healthy Individuals. [9] The use of prescription stimulants is especially prevalent among students attending academic competitive colleges. [13] Surveys suggest that 0.7-4.5% of German students have used cognitive enhancers in their lifetime. [14] [15] [16] Stimulants such as dimethylamylamine and methylphenidate are used on campuses and by younger groups. [9] Based on studies of self-reported illicit stimulant use, 5-35% of college students use diverted ADHD stimulants, Which are primarily used for performance enhancement rather than recreational drugs. [17] [18] [19]

Several factors positively and negatively influence the use of drugs to increase cognitive performance. Among them are the characteristics of the social context. [14] [15] [20] [21]

Side effects

The main concern with pharmaceutical drugs is adverse effects , and these concerns apply to cognitive-enhancing drugs as well. Long-term safety data is typically unavailable for some types of nootropics [9](eg, many non-pharmaceutical cognitive enhancers, newly developed pharmaceuticals and pharmaceuticals with short-term therapeutic use). Racetams -piracetam and other compounds that are structurally related to piracetam -have few serious adverse effects and low toxicity , but there is little evidence that they enhance cognition in individuals without cognitive impairments. [22] [23] While addiction to stimulants is sometimes identified as a cause for concern, [24] a very large body of research on the therapeutic use of the “more addictive” psychostimulants indicate that addiction is fairly rare in therapeutic doses. [25] [26] [27] On their safety profile, a systematic review from June 2015 asserted, “evidence indicates that at low, clinically relevant doses, psychostimulants are devoid of the behavioral and neurochemical actions that define this class of drugs and instead Act widely as cognitive enhancers. ” [28] A systematic review from June 2015 asserted, “evidence indicates that at low, clinically relevant doses, psychostimulants are devoid of the behavioral and neurochemical actions that define this class of drugs and instead act widely as cognitive enhancers.” [28] A systematic review from June 2015 asserted, “evidence indicates that at low, clinically relevant doses, psychostimulants are devoid of the behavioral and neurochemical actions that define this class of drugs and instead act widely as cognitive enhancers.” [28]

In the United States, dietary supplements May be Marketed if the manufacturer can show That It can manufacture the supplement Safely, que la supplement is Indeed generally recognized as safe , and if the manufacturer does not make Any claims about the supplement’s use to treat or prevent prevention Any Disease or condition; Supplements That Contain drugs or for treatment or prevention qui claims are made are illegal under US law. [29]

Drugs

stimulants

In 2015, systematic medical reviews and meta-analyzes of clinical research in humans Established That consensus some stimulants, Only When used at low (therapeutic) concentrations unambiguously Enhance Cognition in the general population; [28] [30] [31] [32] in particular, the classes of stimulants that demonstrate cognition-enhancing effects in humans act as direct agonists or indirect agonists of dopamine receptor D 1 , adrenoceptor A 2 , or both receptors in the prefrontal Cortex. [28] [30] [32] [33] Relatively high doses of stimulants cause cognitive deficits. [32] [33]

Amphetamine Pharmaceuticals (eg, Adderall , dextroamphetamine , and lisdexamfetamine [an inactive prodrug ]) – systematic reviews and meta-analyzes report that amphetamine benefits a range of cognitive functions (eg, inhibitory control , episodic memory , working memory , and aspects of attention ) In the general population, and these effects are especially noticeable in individuals with ADHD. [28] [30] [31] [33] A systematic review from 2014 noted that low doses of amphetamine also improve memory consolidation , in turn leading to Improved recall of information in non-ADHD youth. [31] It also improves task task and performance on tasks that require a high degree of effort. [30] [32] [33]

Methylphenidate – a substituted phenethylamine that improves the range of cognitive functions (eg, working memory , episodic memory , and inhibitory control , aspects of attention and planning latency) in the general population. [28] [30] [31] [34] It also improves task task and performance on tedious tasks that require a high degree of effort. [33] At above optimal doses, methylphenidate has the potential to affect learning by activating neurons in the task at hand. [35]

Nicotine – A meta-analysis of 41 double-blind , placebo -controlled studies concluded that nicotine or smoking had significant positive effects on fine motor abilities, alerting and orienting attention, and episodic and working memory. [40] A 2015 review noted that stimulation of the α4β2 nicotinic receptor is responsible for certain improvements in attentional performance; [41] among the nicotinic receptorsubtypes, nicotine has the highest binding affinity at the α4β2 receptor (k i = 1 nM ), which is also the biological target that mediates nicotine ‘ S addictive properties. [42]

Racetams

Racetams, such as piracetam , oxiracetam , and aniracetam , are structurally similar compounds, which are often marketed as cognitive enhancers and sold over-the-counter . Racetams are often referred to as nootropics, but this property of the drug class is not well established. [43] The racetams have poorly mechanisms of action ; HOWEVER, piracetam and aniracetam are Known to act as positive allosteric modulators of AMPA receptors and APPEAR to modulate cholinergic systems. [44]

According to the US Food and Drug Administration , “Piracetam is not a vitamin, mineral, amino acid, herb or other botanical, or dietary substance for use by the dietary intake. (G) (1) (C) of the Act, 21 USC § 321 (g) (1) (C), because they are not foods and they are intended to affect the structure or any function of the body. (P), because they are not recognized as safe and effective for use under the conditions prescribed, recommended, or suggested in their labeling. “[45]

Miscellaneous

l -Theanine -A-2014 systematic review and meta-analysis on which concurrent caffeine and l -theanine have synergistic effects and promote alertness, attention, andtask switching; [46] These effects are most pronounced during the first hour post-dose. [46]

Atomoxetine – can improve working memory and aspects of attention when used at an optimal dose. [33]

Dietary supplements

Bacopa monnieri – A herb sold as a dietary supplement . There is some preliminary evidence for memory-enhancing effects. [48]

Panax ginseng – A review by the Cochrane. The authors conclude that the efficacy of Panax ginseng in the treatment of gastrointestinal disorders in patients with dementia is very high. [49] According to the National Center for Complementary and Integrative Health “Although Asian ginseng has been widely studied for a variety of uses, research findings to date do not conclusively support health claims associated with herb.” [50] According to a review published in the journal “Advances in Nutrition”, multiple RCTs in healthy volunteers have indicated increases in accuracy of memory, Speed ​​in performing attention tasks and improvement in performing difficult mental arithmetic tasks, as well as reduction in fatigue and improvement in mood. [51]

Ginkgo biloba – An extract of Ginkgo biloba leaf (GBE) is marketed in dietary supplement form with claims it can enhance cognitive function in people without known cognitive problems. Studies have failed to find such effects on memory or attention in healthy people.

Null findings in systematic reviews

Omega-3 fatty acids : DHA and EPA – two Cochrane Collaboration reviews on the use of supplemental omega-3 fatty acids for ADHD and learning disorders. [54] [55] Two other systematic reviews noted no cognition-enhancing effects in the general population or middle-aged and older adults.

Folate – no cognition-enhancing effects in middle-aged and older adults.

The Dextroamphetamine is a psychostimulant drug. It is a non- catecholamine sympathomimetic amine which is the dextrorotatory stereoisomer of the amphetamine molecule . The amphetamine molecule has another stereoisomer: levoamphetamine . Dextroamphetamine is available as a generic drug or under several brands. Dextroamphetamine is often mistakenly called amphetamine, as if it were a synonym, however, it should be remembered that in specialized listings and books the term “amphetamine” refers to a class of stimulants, and “dextroamphetamine” refers to a specific drug Within that class. Continue Reading

Altinicline (SIB-1508Y, SIB-1765F) is a drug that acts as an agonist in nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype. [2] It stimulates the release of dopamine and acetylcholine in the brain in both rodent and primate models, [3] and progressed to Phase II clinical trials for Parkinson’s disease , [4] where “non-antiparkinsonian or cognition enhancement, the effects have been demonstrated,” although its current state is unclear.

Unifiram is an ampakine drug that acts as a positive allosteric modulator of the AMPA receptor , 1 which has been shown to have nootropic effects in animals. 2 3 A series of related compounds are known, one being the sunifiram (DM-235). 4 5 6 This drug has two enantiomers , with (R) – (+) – unifiram acting as more active isomer.

Adderall is a combined drug containing salts of the two enantiomers of amphetamine, a central nervous system (CNS) stimulant of the phenethylamine class. Adderall is used in the treatment of Attention Deficit Hyperactivity Disorder (ADHD) and narcolepsy. It is also used as an athletic performance enhancer and cognitive enhancer, and recreationally as an aphrodisiac and euphoric. The active ingredients of Adderall are 25% levoamphetamine salts (the levogyre or the “left” enantiomer) and 75% dextroamphetamine salts (the dextrogyre or “right” enantiomer).

Adderall is generally well tolerated and effective in treating the symptoms of ADHD and narcolepsy. At therapeutic doses, Adderall causes emotional and cognitive effects such as euphoria, change in sexual desire, increased arousal, and improved cognitive control. At these doses, it induces physical effects such as decreased reaction time, resistance to fatigue and increased muscle strength. On the other hand, much higher doses of Adderall may impair cognitive control, cause rapid muscle degradation, or cause psychosis (eg Delirium and Paranoia). Adderall side effects vary greatly in individuals, but usually include insomnia, dry mouth, and loss of appetite. The risk of developing addiction is insignificant when Adderall is used as prescribed at fairly low daily doses, such as those used to treat ADHD; However, the routine use of Adderall in larger daily doses presents a significant risk of addiction because of the pronounced reinforcing effects present at higher doses. [8] Adderall’s recreational doses are generally much larger than the prescribed therapeutic doses and carry a much higher risk of serious adverse events. [Sources 2] The routine use of Adderall in larger daily doses presents a significant risk of addiction because of the pronounced reinforcement effects that are present at higher doses. [8] Adderall’s recreational doses are generally much larger than the prescribed therapeutic doses and carry a much higher risk of serious adverse events. [Sources 2] The routine use of Adderall in larger daily doses presents a significant risk of addiction because of the pronounced reinforcement effects that are present at higher doses. [8] Adderall’s recreational doses are generally much larger than the prescribed therapeutic doses and carry a much higher risk of serious adverse events. [Sources 2]

The two amphetamine enantiomers that make up Adderall (ie, levoamphetamine and dextro-amphetamine) mitigate the symptoms of ADHD and narcolepsy by increasing the activity of norepinephrine and dopamine neurotransmitters in the brain as a result of their Interactions with the receptor associated with the traces amines 1 (TAAR1) and the transporter of monoamine vesicular 2 (VMAT2) in the neurons. Dextro-amphetamine is a more potent CNS stimulant than levoamphetamine, but levoamphetamine has slightly stronger cardiovascular and peripheral effects and a longer elimination half-life (that is, it remains in the body more Long) than dextro-amphetamine. The Advoverall levoamphetamine component has been reported to improve the response to treatment in some individuals compared to dextroamphetamine alone.

NNI-351 is an active oral inhibitor of DYRK1A and a neurogenesis enhancer that is being developed by NeuroNascent, Inc. for the treatment of Down syndrome, depression and post-traumatic stress disorder (PTSD). [1] [2] Beginning in 2017, it is in the preclinical development phase and has not yet progressed in human clinical trials

The cell transcription factor CREB (cAMP response element binding protein) [1] helps in the learning and stabilization and recovery of long-term memories based on fear. This is mainly due to its expression in the hippocampus and amygdala. Studies that support the role of CREB in cognition include those that eliminate the gene, reduce expression, or overexpress. Continue Reading

The nootropics (from nous mind and tropos bend) or nootropics are drugs , the drugs , plants and various substances having an action of modulation of physiology and psychology involving cognitive increase and that no or relatively little effect Health hazards at standard doses. Nootropics are promoted in transhumanism as a general means of improving living conditions, or for specific purposes, such as increased motivation.

Since the year 2000, more substances (eg, rivastigmine , the galantamine or aniracetam) are used to delay the onset of some cognitive symptoms in Alzheimer’s disease.

Nootropes are drugs extracted from different sources such as the Ginkgo biloba plant . Their effectiveness in diseases such as Alzheimer ‘s disease is not yet proven.

Basmisanil (INN) (developmental code names RG-1662, RO5186582) is a highly selective inverse agonist / negative allosteric modulator of GABA A receptors containing an α 5 subunit developed by Roche for the treatment of cognitive impairments associated with the syndrome Of Down. In August 2015, these are Phase II clinical trials for this indication.